Title: Method for loading lipsomes with ionizable phosphorylated hydrophobic compounds, pharmaceutical preparations and a method for administering the preparations

Abstract

A method of entrapping ionizable compounds, preferably phosphorylated hydrophobic compounds, into liposomes having transmembrane gradients is disclosed. The procedures involve forming liposomes in an acidic medium or a basic medium, adding to the acidic medium a cationic compound or to the basic medium an anionic compound and then adding a base to the cationic-containing medium or an acid to the anionic-containing medium, thereby inducing the ionizable compound into the liposomes' internal aqueous phase. The compound-entrapped liposomes prepared in accordance with the disclosed methods may be used as pharmaceutical preparations. Methods of administering such pharmaceutical preparations are also disclosed.

Inventors:

Mehlhorn, Rolf Joachim ^[1]

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1. Richmond, CA

Issue Date:

1998-10-27

Research Org.:

Lawrence Berkeley National Laboratory (LBNL), Berkeley, CA (United States)

OSTI Identifier:

879398

Patent Number(s):

5827532

Application Number:

08/791557

Assignee:

The Reagents of the University of California (Oakland, CA)

Patent Classifications (CPCs):

A - HUMAN NECESSITIES A61 - MEDICAL OR VETERINARY SCIENCE A61K - PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

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A - HUMAN NECESSITIES A61 - MEDICAL OR VETERINARY SCIENCE A61K - PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

A61K9/1278 - {Post-loading, e.g. by ion or pH gradient}

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DOE Contract Number:  

AC03-76SF00098

Resource Type:

Patent

Country of Publication:

United States

Language:

English